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Development of molecular probes for the human 5-HT6 receptor

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dc.contributor.authorVázquez Villa, María Del Henar
dc.contributor.authorGonzález Vera, Juan Antonio
dc.contributor.authorBenhamú Salama, Bellinda
dc.contributor.authorViso, Alma
dc.contributor.authorFernandez de la Pradilla, Roberto
dc.contributor.authorJunquera González, María Elena
dc.contributor.authorAicart Sospedra, Emilio
dc.contributor.authorLópez Rodríguez, María Luz
dc.contributor.authorOrtega Gutiérrez, Silvia
dc.date.accessioned2025-01-15T17:29:03Z
dc.date.available2025-01-15T17:29:03Z
dc.date.issued2010-10-14
dc.description.abstractIn this work we report the synthesis of a set of labeled ligands targeting the human 5-HT6 receptor (h5-HT6R). Among the synthesized compounds, fluorescent probe 10 (Ki = 175 nM and Φf = 0.21) and biotinylated derivative 15 (Ki = 90 nM) deserve special attention because they enable direct observation of the h5-HT6R in cells. Thus, they represent the first molecular probes for 5-HT6R visualization. These results are the starting point for introducing a variety of tags in these or other 5-HT6R ligand scaffolds aimed at the development of optimized probes with tailored profiles in terms of fluorescence, affinity, or selectivity.
dc.description.departmentDepto. de Química Orgánica
dc.description.facultyFac. de Ciencias Químicas
dc.description.refereedTRUE
dc.description.sponsorshipMinisterio de Ciencia e Innovación
dc.description.sponsorshipComunidad de Madrid
dc.description.statuspub
dc.identifier.citationVázquez-Villa, H., González-Vera, J. A., Benhamú, B., Viso, A., Fernández de la Pradilla, R., Junquera, E., Aicart, E., López-Rodríguez, M. L., Ortega-Gutiérrez, S. Development of Molecular Probes for the Human 5-HT6 Receptor. J. Med. Chem. 2010, 53 (19), 7095-7106
dc.identifier.doi10.1021/jm1007177
dc.identifier.essn1520-4804
dc.identifier.issn0022-2623
dc.identifier.officialurlhttps://doi.org/10.1021/jm1007177
dc.identifier.urihttps://hdl.handle.net/20.500.14352/114528
dc.issue.number19
dc.journal.titleJournal of Medicinal Chemistry
dc.language.isoeng
dc.page.final7106
dc.page.initial7095
dc.publisherACS Publications
dc.relation.projectIDSAF-2007/67008-C02-01
dc.relation.projectIDCTQ2009-07752
dc.relation.projectIDinfo:eu-repo/grantAgreement/MICINN//FIS2008-06197-C02-01/ES/NANOCOMPACTACION COLOIDAL DEL ADN: UNA APROXIMACION EXPERIMENTAL Y TEORICA/
dc.relation.projectIDSAF-2010/ 22198-C02-01
dc.relation.projectIDS-SAL-249-2006
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internationalen
dc.rights.accessRightsrestricted access
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/
dc.subject.cdu547
dc.subject.keywordSerotonin 5-HT6 receptor
dc.subject.keywordGPCR
dc.subject.keywordMolecular probes
dc.subject.keywordReceptor visualization
dc.subject.ucmQuímica orgánica (Química)
dc.subject.unesco2306 Química Orgánica
dc.subject.unesco2390.01 Diseño. Síntesis y Estudio Nuevos Fármacos
dc.titleDevelopment of molecular probes for the human 5-HT6 receptor
dc.typejournal article
dc.type.hasVersionAM
dc.volume.number53
dspace.entity.typePublication
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